HRP20151430T1 - Pyridine and pyrazine derivative for the treatment of cf - Google Patents
Pyridine and pyrazine derivative for the treatment of cf Download PDFInfo
- Publication number
- HRP20151430T1 HRP20151430T1 HRP20151430TT HRP20151430T HRP20151430T1 HR P20151430 T1 HRP20151430 T1 HR P20151430T1 HR P20151430T T HRP20151430T T HR P20151430TT HR P20151430 T HRP20151430 T HR P20151430T HR P20151430 T1 HRP20151430 T1 HR P20151430T1
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- optionally substituted
- trifluoromethyl
- amino
- amide
- Prior art date
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- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 title 2
- 150000003216 pyrazines Chemical class 0.000 title 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 52
- 125000005843 halogen group Chemical group 0.000 claims 34
- 125000000217 alkyl group Chemical group 0.000 claims 27
- 125000005842 heteroatom Chemical group 0.000 claims 23
- 229910052760 oxygen Inorganic materials 0.000 claims 23
- 229910052717 sulfur Inorganic materials 0.000 claims 23
- 125000001424 substituent group Chemical group 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 18
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 17
- 150000002367 halogens Chemical group 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 14
- 125000003118 aryl group Chemical group 0.000 claims 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 8
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 7
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 125000004043 oxo group Chemical group O=* 0.000 claims 5
- -1 R 14 Chemical compound 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- 125000005330 8 membered heterocyclic group Chemical group 0.000 claims 3
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 3
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- UWWNIBQLEBYWJZ-UHFFFAOYSA-N 3-amino-5,6-bis(trifluoromethyl)pyridine-2-carboxylic acid Chemical compound NC1=CC(C(F)(F)F)=C(C(F)(F)F)N=C1C(O)=O UWWNIBQLEBYWJZ-UHFFFAOYSA-N 0.000 claims 2
- TZBFDPNSDFVMAL-UHFFFAOYSA-N 3-amino-6-(4-fluorophenyl)-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NCC(O)(C)C(F)(F)F)=NC(C=2C=CC(F)=CC=2)=C1C(F)(F)F TZBFDPNSDFVMAL-UHFFFAOYSA-N 0.000 claims 2
- HZEFBJDLLZEVBS-UHFFFAOYSA-N 3-amino-6-(6-methylpyridin-3-yl)-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=NC(C)=CC=C1C1=NC(C(=O)NCC(C)(O)C(F)(F)F)=C(N)C=C1C(F)(F)F HZEFBJDLLZEVBS-UHFFFAOYSA-N 0.000 claims 2
- USHQRIKZLHNPQR-SNVBAGLBSA-N 3-amino-6-methoxy-n-[(2r)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC1=NC(C(=O)NC[C@@](C)(O)C(F)(F)F)=C(N)C=C1C(F)(F)F USHQRIKZLHNPQR-SNVBAGLBSA-N 0.000 claims 2
- USHQRIKZLHNPQR-JTQLQIEISA-N 3-amino-6-methoxy-n-[(2s)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC1=NC(C(=O)NC[C@](C)(O)C(F)(F)F)=C(N)C=C1C(F)(F)F USHQRIKZLHNPQR-JTQLQIEISA-N 0.000 claims 2
- 125000005915 C6-C14 aryl group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 230000036571 hydration Effects 0.000 claims 2
- 238000006703 hydration reaction Methods 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 230000000414 obstructive effect Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 210000002345 respiratory system Anatomy 0.000 claims 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- WHFKKQOPYKKTRR-UHFFFAOYSA-N 3-amino-6-(1,3-oxazol-2-yl)-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NCC(O)(C)C(F)(F)F)=NC(C=2OC=CN=2)=C1C(F)(F)F WHFKKQOPYKKTRR-UHFFFAOYSA-N 0.000 claims 1
- UFCJPGYFNTWEJU-UHFFFAOYSA-N 3-amino-6-(1-methylpyrazol-4-yl)-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=NN(C)C=C1C1=NC(C(=O)NCC(C)(O)C(F)(F)F)=C(N)C=C1C(F)(F)F UFCJPGYFNTWEJU-UHFFFAOYSA-N 0.000 claims 1
- KGUOYCPINMKTEY-UHFFFAOYSA-N 3-amino-6-(2,4-dichlorophenyl)-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NCC(O)(C)C(F)(F)F)=NC(C=2C(=CC(Cl)=CC=2)Cl)=C1C(F)(F)F KGUOYCPINMKTEY-UHFFFAOYSA-N 0.000 claims 1
- QSUKHXHXEOGZBK-GFCCVEGCSA-N 3-amino-6-(4-chloro-2-methylphenyl)-n-[(2r)-3,3,3-trifluoro-2-hydroxypropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound CC1=CC(Cl)=CC=C1C1=NC(C(=O)NC[C@@H](O)C(F)(F)F)=C(N)C=C1C(F)(F)F QSUKHXHXEOGZBK-GFCCVEGCSA-N 0.000 claims 1
- GJQPKGWZJDQMIQ-UHFFFAOYSA-N 3-amino-6-(4-fluorophenyl)-n-(2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NCC(C)(O)C)=NC(C=2C=CC(F)=CC=2)=C1C(F)(F)F GJQPKGWZJDQMIQ-UHFFFAOYSA-N 0.000 claims 1
- TZBFDPNSDFVMAL-OAHLLOKOSA-N 3-amino-6-(4-fluorophenyl)-n-[(2r)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NC[C@](O)(C)C(F)(F)F)=NC(C=2C=CC(F)=CC=2)=C1C(F)(F)F TZBFDPNSDFVMAL-OAHLLOKOSA-N 0.000 claims 1
- TZBFDPNSDFVMAL-HNNXBMFYSA-N 3-amino-6-(4-fluorophenyl)-n-[(2s)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NC[C@@](O)(C)C(F)(F)F)=NC(C=2C=CC(F)=CC=2)=C1C(F)(F)F TZBFDPNSDFVMAL-HNNXBMFYSA-N 0.000 claims 1
- SFKNCCQBPWDVKN-UHFFFAOYSA-N 3-amino-6-bromo-n-(1,3-dioxolan-2-ylmethyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NCC1OCCO1 SFKNCCQBPWDVKN-UHFFFAOYSA-N 0.000 claims 1
- GVRZCDPWQYZXNS-UHFFFAOYSA-N 3-amino-6-bromo-n-(2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound CC(C)(O)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N GVRZCDPWQYZXNS-UHFFFAOYSA-N 0.000 claims 1
- OPLNZGRSQIIIAO-UHFFFAOYSA-N 3-amino-6-bromo-n-(2-hydroxypropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound CC(O)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N OPLNZGRSQIIIAO-UHFFFAOYSA-N 0.000 claims 1
- ZYWMZMYAYYWCDE-UHFFFAOYSA-N 3-amino-6-bromo-n-(2-methoxyethyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COCCNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N ZYWMZMYAYYWCDE-UHFFFAOYSA-N 0.000 claims 1
- RIMPMQYAYQSIRX-UHFFFAOYSA-N 3-amino-6-bromo-n-(2-methyl-2-piperidin-1-ylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1CCCCN1C(C)(C)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N RIMPMQYAYQSIRX-UHFFFAOYSA-N 0.000 claims 1
- PRICOGDBMOXKKB-UHFFFAOYSA-N 3-amino-6-bromo-n-(2-morpholin-4-yl-2-phenylethyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NCC(C=1C=CC=CC=1)N1CCOCC1 PRICOGDBMOXKKB-UHFFFAOYSA-N 0.000 claims 1
- FKVGABLCWNRNCT-UHFFFAOYSA-N 3-amino-6-bromo-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound FC(F)(F)C(O)(C)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N FKVGABLCWNRNCT-UHFFFAOYSA-N 0.000 claims 1
- HMTZYEHOLZSQKH-UHFFFAOYSA-N 3-amino-6-bromo-n-(3,3,3-trifluoro-2-hydroxypropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NCC(O)C(F)(F)F HMTZYEHOLZSQKH-UHFFFAOYSA-N 0.000 claims 1
- IZNGGIWWUGSTJK-UHFFFAOYSA-N 3-amino-6-bromo-n-(3,3,3-trifluoro-2-methoxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC(C)(C(F)(F)F)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N IZNGGIWWUGSTJK-UHFFFAOYSA-N 0.000 claims 1
- FBKLGQNLLLOCOC-UHFFFAOYSA-N 3-amino-6-bromo-n-(3-methyl-2-oxobutyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound CC(C)C(=O)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N FBKLGQNLLLOCOC-UHFFFAOYSA-N 0.000 claims 1
- IXGCWTUELRQRAE-UHFFFAOYSA-N 3-amino-6-bromo-n-(oxolan-2-ylmethyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NCC1OCCC1 IXGCWTUELRQRAE-UHFFFAOYSA-N 0.000 claims 1
- VJSZJLMTQKHBKQ-UHFFFAOYSA-N 3-amino-6-bromo-n-[(2-methyloxolan-2-yl)methyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound N=1C(Br)=C(C(F)(F)F)C=C(N)C=1C(=O)NCC1(C)CCCO1 VJSZJLMTQKHBKQ-UHFFFAOYSA-N 0.000 claims 1
- FKVGABLCWNRNCT-SECBINFHSA-N 3-amino-6-bromo-n-[(2r)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound FC(F)(F)[C@@](O)(C)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N FKVGABLCWNRNCT-SECBINFHSA-N 0.000 claims 1
- FKVGABLCWNRNCT-VIFPVBQESA-N 3-amino-6-bromo-n-[(2s)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound FC(F)(F)[C@](O)(C)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N FKVGABLCWNRNCT-VIFPVBQESA-N 0.000 claims 1
- HMTZYEHOLZSQKH-YFKPBYRVSA-N 3-amino-6-bromo-n-[(2s)-3,3,3-trifluoro-2-hydroxypropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NC[C@H](O)C(F)(F)F HMTZYEHOLZSQKH-YFKPBYRVSA-N 0.000 claims 1
- KABJGLMCDHJSJB-UHFFFAOYSA-N 3-amino-6-bromo-n-[2-(4-fluorophenyl)-2-morpholin-4-ylethyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NCC(C=1C=CC(F)=CC=1)N1CCOCC1 KABJGLMCDHJSJB-UHFFFAOYSA-N 0.000 claims 1
- RZHBHISYYNDQRR-UHFFFAOYSA-N 3-amino-6-bromo-n-[2-(dimethylamino)-2-phenylethyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C=1C=CC=CC=1C(N(C)C)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N RZHBHISYYNDQRR-UHFFFAOYSA-N 0.000 claims 1
- CJMBGYUOORNPLR-UHFFFAOYSA-N 3-amino-6-bromo-n-[3,3,3-trifluoro-2-hydroxy-2-(trifluoromethyl)propyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NCC(O)(C(F)(F)F)C(F)(F)F CJMBGYUOORNPLR-UHFFFAOYSA-N 0.000 claims 1
- IXGCWTUELRQRAE-ZCFIWIBFSA-N 3-amino-6-bromo-n-[[(2r)-oxolan-2-yl]methyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NC[C@@H]1OCCC1 IXGCWTUELRQRAE-ZCFIWIBFSA-N 0.000 claims 1
- IXGCWTUELRQRAE-LURJTMIESA-N 3-amino-6-bromo-n-[[(2s)-oxolan-2-yl]methyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NC[C@H]1OCCC1 IXGCWTUELRQRAE-LURJTMIESA-N 0.000 claims 1
- JUKULCRENGDXKQ-UHFFFAOYSA-N 3-amino-6-cyclopropyl-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NCC(O)(C)C(F)(F)F)=NC(C2CC2)=C1C(F)(F)F JUKULCRENGDXKQ-UHFFFAOYSA-N 0.000 claims 1
- QOLIZSVOBMCSPJ-NSHDSACASA-N 3-amino-6-ethoxy-n-[(2s)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound CCOC1=NC(C(=O)NC[C@](C)(O)C(F)(F)F)=C(N)C=C1C(F)(F)F QOLIZSVOBMCSPJ-NSHDSACASA-N 0.000 claims 1
- USHQRIKZLHNPQR-UHFFFAOYSA-N 3-amino-6-methoxy-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC1=NC(C(=O)NCC(C)(O)C(F)(F)F)=C(N)C=C1C(F)(F)F USHQRIKZLHNPQR-UHFFFAOYSA-N 0.000 claims 1
- SGMQDTWKBCOQTJ-UHFFFAOYSA-N 3-amino-6-methoxy-n-(3,3,3-trifluoro-2-hydroxypropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC1=NC(C(=O)NCC(O)C(F)(F)F)=C(N)C=C1C(F)(F)F SGMQDTWKBCOQTJ-UHFFFAOYSA-N 0.000 claims 1
- JLZLMMKWPPNUJJ-UHFFFAOYSA-N 3-amino-6-methoxy-n-[3,3,3-trifluoro-2-[(4-methoxyphenyl)methylamino]-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=CC(OC)=CC=C1CNC(C)(C(F)(F)F)CNC(=O)C1=NC(OC)=C(C(F)(F)F)C=C1N JLZLMMKWPPNUJJ-UHFFFAOYSA-N 0.000 claims 1
- IGGKDUGORVNOGN-UHFFFAOYSA-N 3-amino-6-methoxy-n-[3,3,3-trifluoro-2-hydroxy-2-(trifluoromethyl)propyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC1=NC(C(=O)NCC(O)(C(F)(F)F)C(F)(F)F)=C(N)C=C1C(F)(F)F IGGKDUGORVNOGN-UHFFFAOYSA-N 0.000 claims 1
- HQGQMJKYAPMBRQ-UHFFFAOYSA-N 3-amino-6-pyridin-4-yl-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NCC(O)(C)C(F)(F)F)=NC(C=2C=CN=CC=2)=C1C(F)(F)F HQGQMJKYAPMBRQ-UHFFFAOYSA-N 0.000 claims 1
- NMXSTLHGFBNGMD-UHFFFAOYSA-N 3-amino-6-pyrrolidin-1-yl-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NCC(O)(C)C(F)(F)F)=NC(N2CCCC2)=C1C(F)(F)F NMXSTLHGFBNGMD-UHFFFAOYSA-N 0.000 claims 1
- VJOIAFQFVKJERR-UHFFFAOYSA-N 3-amino-n-(2-amino-3,3,3-trifluoro-2-methylpropyl)-6-methoxy-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC1=NC(C(=O)NCC(C)(N)C(F)(F)F)=C(N)C=C1C(F)(F)F VJOIAFQFVKJERR-UHFFFAOYSA-N 0.000 claims 1
- POGTUVIIGKHISG-UHFFFAOYSA-N 3-amino-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound FC(F)(F)C(O)(C)CNC(=O)C1=NC=C(C(F)(F)F)C=C1N POGTUVIIGKHISG-UHFFFAOYSA-N 0.000 claims 1
- DOVVSHMLCFFGGB-SECBINFHSA-N 3-amino-n-[(2r)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5,6-bis(trifluoromethyl)pyridine-2-carboxamide Chemical compound FC(F)(F)[C@@](O)(C)CNC(=O)C1=NC(C(F)(F)F)=C(C(F)(F)F)C=C1N DOVVSHMLCFFGGB-SECBINFHSA-N 0.000 claims 1
- DOVVSHMLCFFGGB-VIFPVBQESA-N 3-amino-n-[(2s)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5,6-bis(trifluoromethyl)pyridine-2-carboxamide Chemical compound FC(F)(F)[C@](O)(C)CNC(=O)C1=NC(C(F)(F)F)=C(C(F)(F)F)C=C1N DOVVSHMLCFFGGB-VIFPVBQESA-N 0.000 claims 1
- CMFXZGDPYQFXMK-UHFFFAOYSA-N 3-amino-n-[2-hydroxy-3-methyl-2-(trifluoromethyl)butyl]-6-methoxy-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC1=NC(C(=O)NCC(O)(C(C)C)C(F)(F)F)=C(N)C=C1C(F)(F)F CMFXZGDPYQFXMK-UHFFFAOYSA-N 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940088710 antibiotic agent Drugs 0.000 claims 1
- 229940125715 antihistaminic agent Drugs 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 239000003434 antitussive agent Substances 0.000 claims 1
- 229940124584 antitussives Drugs 0.000 claims 1
- 229940124630 bronchodilator Drugs 0.000 claims 1
- 239000000168 bronchodilator agent Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000002713 epithelial sodium channel blocking agent Substances 0.000 claims 1
- DUZCWGDFTIWAOZ-UHFFFAOYSA-N methyl 3-[[3-amino-6-bromo-5-(trifluoromethyl)pyridine-2-carbonyl]amino]propanoate Chemical compound COC(=O)CCNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N DUZCWGDFTIWAOZ-UHFFFAOYSA-N 0.000 claims 1
- 239000002357 osmotic agent Substances 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
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Claims (18)
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PCT/EP2011/054038 WO2011113894A1 (en) | 2010-03-19 | 2011-03-17 | Pyridine and pyrazine derivative for the treatment of cf |
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US6858615B2 (en) | 2002-02-19 | 2005-02-22 | Parion Sciences, Inc. | Phenyl guanidine sodium channel blockers |
US8247436B2 (en) | 2010-03-19 | 2012-08-21 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of CF |
AR086745A1 (en) | 2011-06-27 | 2014-01-22 | Parion Sciences Inc | 3,5-DIAMINO-6-CHLORINE-N- (N- (4- (4- (2- (HEXIL (2,3,4,5,6-PENTAHYDROXIHEXIL)) AMINO) ETOXI) PHENYL) BUTIL) CARBAMIMIDOIL) PIRAZINA -2-CARBOXAMIDE |
FI2753632T3 (en) | 2011-09-08 | 2023-08-02 | Sage Therapeutics Inc | Neuroactive steroids, compositions, and uses thereof |
WO2013038378A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Pyridine amide derivatives |
WO2013038381A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Pyridine/pyrazine amide derivatives |
JP6165733B2 (en) | 2011-09-16 | 2017-07-19 | ノバルティス アーゲー | N-substituted heterocyclylcarboxamides |
WO2013038373A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Pyridine amide derivatives |
US9181185B2 (en) | 2011-10-31 | 2015-11-10 | Purdue Pharma L.P. | Heteroaryl compounds as sodium channel blockers |
SG10201606135TA (en) | 2012-01-25 | 2016-09-29 | Vertex Pharma | Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
SI2914248T2 (en) | 2012-11-02 | 2023-12-29 | Vertex Pharmaceuticals Incorporated, | Pharmaceutical compositions for the treatment of cftr mediated diseases |
DK2931713T3 (en) | 2012-12-17 | 2017-01-30 | Parion Sciences Inc | CHLORPYRAZINE CARBOXAMIDE DERIVATIVES USED FOR THE TREATMENT OF DISEASES BENEFITED BY INDEPENDENT MOSPHEREWIN |
RU2018138195A (en) | 2012-12-17 | 2018-12-18 | Пэрион Сайенсиз, Инк. | COMPOUNDS 3,5-DIAMINO-6-CHLORO-N- (N- (4-Phenylbutyl) Carbamimidoyl) Pyrazine-2-Carboxamide |
WO2014100719A2 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
JP2016505000A (en) | 2012-12-21 | 2016-02-18 | エピザイム,インコーポレイティド | PRMT5 inhibitors and uses thereof |
US9745291B2 (en) | 2012-12-21 | 2017-08-29 | Epizyme, Inc. | PRMT5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof |
US10118918B2 (en) | 2012-12-21 | 2018-11-06 | Epizyme, Inc. | PRMT5 inhibitors and uses thereof |
US9611257B2 (en) | 2012-12-21 | 2017-04-04 | Epizyme, Inc. | PRMT5 inhibitors and uses thereof |
PT3461834T (en) | 2013-03-13 | 2021-09-10 | Sage Therapeutics Inc | Neuroactive steroids |
WO2014141064A1 (en) | 2013-03-13 | 2014-09-18 | Novartis Ag | Notch2 binding molecules for treating respiratory diseases |
NZ718430A (en) | 2013-10-04 | 2021-12-24 | Infinity Pharmaceuticals Inc | Heterocyclic compounds and uses thereof |
US9751888B2 (en) | 2013-10-04 | 2017-09-05 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US9102633B2 (en) | 2013-12-13 | 2015-08-11 | Parion Sciences, Inc. | Arylalkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds |
CN113620958A (en) | 2014-03-19 | 2021-11-09 | 无限药品股份有限公司 | Heterocyclic compounds for the treatment of PI 3K-gamma mediated disorders |
SI3925607T1 (en) | 2014-04-15 | 2023-10-30 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases |
EP2932966A1 (en) | 2014-04-16 | 2015-10-21 | Novartis AG | Gamma secretase inhibitors for treating respiratory diseases |
CA2945212A1 (en) | 2014-04-24 | 2015-10-29 | Novartis Ag | Amino pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors |
WO2015195967A1 (en) | 2014-06-18 | 2015-12-23 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
EP3157917B1 (en) | 2014-06-19 | 2020-03-18 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr activity |
WO2016022605A1 (en) | 2014-08-04 | 2016-02-11 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
US9708348B2 (en) | 2014-10-03 | 2017-07-18 | Infinity Pharmaceuticals, Inc. | Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof |
EP3798214B1 (en) | 2014-10-06 | 2022-09-14 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
AU2015339196A1 (en) | 2014-10-31 | 2017-05-11 | Abbvie S.A.R.L. | Substituted tetrahydropyrans and method of use |
US10392378B2 (en) | 2014-12-23 | 2019-08-27 | Proteostasis Therapeutics, Inc. | Derivatives of 5-phenyl- or 5-heteroarylathiazol-2-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
MA41253A (en) | 2014-12-23 | 2017-10-31 | Proteostasis Therapeutics Inc | COMPOUNDS, COMPOSITIONS AND PROCESSES TO INCREASE THE ACTIVITY OF CFTR |
WO2016105468A1 (en) | 2014-12-23 | 2016-06-30 | Proteostasis Therapeutics, Inc. | Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
CN107922338A (en) * | 2015-06-02 | 2018-04-17 | 艾伯维公司 | The pyridine and application method being substituted |
IL256710B2 (en) | 2015-07-06 | 2024-01-01 | Sage Therapeutics Inc | Oxysterols and methods of use thereof |
SG10202002655VA (en) | 2015-07-06 | 2020-05-28 | Sage Therapeutics Inc | Oxysterols and methods of use thereof |
MA42409A (en) | 2015-07-06 | 2018-05-16 | Sage Therapeutics Inc | OXYSTEROLS AND THEIR METHODS OF USE |
US9840513B2 (en) | 2015-07-16 | 2017-12-12 | Abbvie S.Á.R.L. | Substituted tricyclics and method of use |
WO2017019589A1 (en) | 2015-07-24 | 2017-02-02 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr activity |
CA2998469A1 (en) | 2015-09-14 | 2017-03-23 | Infinity Pharmaceuticals, Inc. | Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same |
AU2016333907A1 (en) | 2015-10-09 | 2018-04-12 | AbbVie S.à.r.l. | Novel compounds for treatment of cystic fibrosis |
MX2018004364A (en) | 2015-10-09 | 2018-08-16 | Abbvie Sarl | Substituted pyrazolo[3,4-b]pyridin-6-carboxylic acids and their use. |
BR112018007161B1 (en) | 2015-10-09 | 2024-01-16 | Galapagos Nv | PYRAZOLO[3,4-b]PYRIDIN-6-CARBOXAMIDE N-SULFONYLATED COMPOUNDS, PHARMACEUTICAL COMPOSITION CONTAINING SAID COMPOUNDS AND USES THEREOF TO TREAT CYSTIC FIBROSIS |
US10759806B2 (en) | 2016-03-17 | 2020-09-01 | Infinity Pharmaceuticals, Inc. | Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors |
SI3436022T1 (en) | 2016-04-01 | 2022-08-31 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
WO2017177124A1 (en) | 2016-04-07 | 2017-10-12 | Proteostasis Therapeutics, Inc. | Silicone atoms containing ivacaftor analogues |
CA3016303A1 (en) | 2016-04-26 | 2017-11-02 | Abbvie S.A.R.L. | Modulators of cystic fibrosis transmembrane conductance regulator protein |
US10752653B2 (en) | 2016-05-06 | 2020-08-25 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
US10138227B2 (en) * | 2016-06-03 | 2018-11-27 | Abbvie S.Á.R.L. | Heteroaryl substituted pyridines and methods of use |
US10919914B2 (en) | 2016-06-08 | 2021-02-16 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
GB201610854D0 (en) | 2016-06-21 | 2016-08-03 | Entpr Therapeutics Ltd | Compounds |
MA45397A (en) | 2016-06-21 | 2019-04-24 | Proteostasis Therapeutics Inc | COMPOUNDS, COMPOSITIONS AND PROCESSES TO INCREASE THE ACTIVITY OF CFTR |
PL3481846T3 (en) | 2016-07-07 | 2021-12-20 | Sage Therapeutics, Inc. | 11-substituted 24-hydroxysterols for use in the treatment of nmda related conditions |
EP3519422B1 (en) | 2016-09-30 | 2022-08-31 | Sage Therapeutics, Inc. | C7 substituted oxysterols and these compounds for use as nmda modulators |
HUE056716T2 (en) * | 2016-09-30 | 2022-03-28 | Vertex Pharma | Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
US9981910B2 (en) * | 2016-10-07 | 2018-05-29 | Abbvie S.Á.R.L. | Substituted pyrrolidines and methods of use |
US10399940B2 (en) | 2016-10-07 | 2019-09-03 | Abbvie S.Á.R.L. | Substituted pyrrolidines and methods of use |
CN110072874B (en) | 2016-10-18 | 2022-08-12 | 萨奇治疗股份有限公司 | Oxysterol and methods of use thereof |
RU2019115113A (en) | 2016-10-18 | 2020-11-24 | Сейдж Терапьютикс, Инк. | OXYSTEROLES AND METHODS OF THEIR APPLICATION |
WO2018081377A1 (en) | 2016-10-26 | 2018-05-03 | Proteostasis Therapeutics, Inc. | N-phenyl-2-(3-phenyl-6-oxo-1,6-dihydropyridazin-1-yl)acetamide derivatives for treating cystic fibrosis |
WO2018081381A1 (en) | 2016-10-26 | 2018-05-03 | Proteostasis Therapeutics, Inc | Pyridazine derivatives, compositions and methods for modulating cftr |
CA3041811A1 (en) | 2016-10-26 | 2018-05-03 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating cftr |
GB201619694D0 (en) | 2016-11-22 | 2017-01-04 | Entpr Therapeutics Ltd | Compounds |
CA3044366A1 (en) * | 2016-12-19 | 2018-06-28 | Novartis Ag | New picolinic acid derivatives and their use as intermediates |
US20200123137A1 (en) | 2016-12-20 | 2020-04-23 | AbbVie S.à.r.l. | Deuterated cftr modulators and methods of use |
TW201831471A (en) | 2017-02-24 | 2018-09-01 | 盧森堡商艾伯維公司 | Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use |
CA3061476A1 (en) | 2017-04-28 | 2018-11-01 | Proteostasis Therapeutics, Inc. | 4-sulfonylaminocarbonylquinoline derivatives for increasing cftr activity |
US10988454B2 (en) | 2017-09-14 | 2021-04-27 | Abbvie Overseas S.À.R.L. | Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use |
EP3691638A1 (en) | 2017-10-06 | 2020-08-12 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods for increasing cftr activity |
GB201717051D0 (en) | 2017-10-17 | 2017-11-29 | Enterprise Therapeutics Ltd | Compounds |
US20190210973A1 (en) | 2018-01-05 | 2019-07-11 | The Curators Of The University Of Missouri | Compounds and methods for treatment of cystic fibrosis |
WO2019193062A1 (en) | 2018-04-03 | 2019-10-10 | Abbvie S.Á.R.L | Substituted pyrrolidines and their use |
GB201808093D0 (en) | 2018-05-18 | 2018-07-04 | Enterprise Therapeutics Ltd | Compounds |
US11345691B2 (en) | 2019-06-03 | 2022-05-31 | AbbVie Global Enterprises Ltd. | Prodrug modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use |
MX2021015133A (en) * | 2019-06-10 | 2022-01-24 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of cf, copd, and bronchiectasis. |
TW202115014A (en) | 2019-07-12 | 2021-04-16 | 美商奧佛麥德公司 | Compound for treating cystic fibrosis |
KR20220035421A (en) | 2019-07-15 | 2022-03-22 | 노파르티스 아게 | Formulation of (S)-3-amino-6-methoxy-N-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)picolinamide |
WO2021097054A1 (en) | 2019-11-12 | 2021-05-20 | Genzyme Corporation | 6-membered heteroarylaminosulfonamides for treating diseases and conditions mediated by deficient cftr activity |
WO2021113806A1 (en) | 2019-12-05 | 2021-06-10 | Genzyme Corporation | Arylamides and methods of use thereof |
WO2021113809A1 (en) | 2019-12-05 | 2021-06-10 | Genzyme Corporation | Arylamides and methods of use thereof |
EP4211171A2 (en) | 2020-09-10 | 2023-07-19 | Precirix N.V. | Antibody fragment against fap |
WO2022150173A1 (en) | 2021-01-06 | 2022-07-14 | AbbVie Global Enterprises Ltd. | Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use |
US20220211692A1 (en) | 2021-01-06 | 2022-07-07 | AbbVie Global Enterprises Ltd. | Modulators of the Cystic Fibrosis Transmembrane Conductance Regulator Protein and Methods of Use |
AU2022265718A1 (en) | 2021-04-29 | 2023-11-02 | Novartis Ag | Deubiquitinase-targeting chimeras and related methods |
JP2024533216A (en) | 2021-09-03 | 2024-09-12 | ジェンザイム・コーポレーション | Indole compounds and methods of use |
EP4396176A1 (en) | 2021-09-03 | 2024-07-10 | Genzyme Corporation | Indole compounds and uses thereof in the treatement of cystic fibrosis |
WO2023109939A1 (en) * | 2021-12-17 | 2023-06-22 | 苏州晶云药物科技股份有限公司 | Crystal form of pyridine derivative and preparation method therefor |
WO2023203135A1 (en) | 2022-04-22 | 2023-10-26 | Precirix N.V. | Improved radiolabelled antibody |
WO2023213801A1 (en) | 2022-05-02 | 2023-11-09 | Precirix N.V. | Pre-targeting |
WO2024054851A1 (en) | 2022-09-07 | 2024-03-14 | Sionna Therapeutics | Macrocyclic compounds, compositions and methods of using thereof |
WO2024054840A1 (en) | 2022-09-07 | 2024-03-14 | Sionna Therapeutics | Macrocyclic compounds, compositions, and methods of using thereof |
WO2024054845A1 (en) | 2022-09-07 | 2024-03-14 | Sionna Therapeutics | Macrocycic compounds, compositions, and methods of using thereof |
WO2024056798A1 (en) | 2022-09-15 | 2024-03-21 | Idorsia Pharmaceuticals Ltd | Macrocyclic cftr modulators |
TW202421102A (en) | 2022-09-15 | 2024-06-01 | 瑞士商愛杜西亞製藥有限公司 | Combination of macrocyclic cftr modulators with cftr correctors and/or cftr potentiators |
Family Cites Families (188)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE31894C (en) | E. j SATTLER in Königshütte O. S | Valve for water post | ||
NL299931A (en) | 1962-10-30 | |||
US3527758A (en) | 1967-04-13 | 1970-09-08 | Merck & Co Inc | Process for the preparation of pyrazinoylguanidines from a pyrazinoic azide and a guanidine |
GB1219606A (en) | 1968-07-15 | 1971-01-20 | Rech S Et D Applic Scient Soge | Quinuclidinol derivatives and preparation thereof |
CA927163A (en) | 1969-12-04 | 1973-05-29 | W. Appol David | Picker for divellicating pulp |
JPS6235216A (en) | 1985-08-09 | 1987-02-16 | Noritoshi Nakabachi | Method and device for measuring thickness of heterogeneous material layer nondestructively |
GB8908875D0 (en) | 1989-04-19 | 1989-06-07 | Ici Plc | Fungicides |
GB8923590D0 (en) | 1989-10-19 | 1989-12-06 | Pfizer Ltd | Antimuscarinic bronchodilators |
PT100441A (en) | 1991-05-02 | 1993-09-30 | Smithkline Beecham Corp | PIRROLIDINONES, ITS PREPARATION PROCESS, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND USE |
WO1993018007A1 (en) | 1992-03-13 | 1993-09-16 | Tokyo Tanabe Company Limited | Novel carbostyril derivative |
CZ283425B6 (en) | 1992-04-02 | 1998-04-15 | Smithkline Beecham Corporation | Phenyl derivatives and pharmaceutical compositions containing thereof |
WO1993019750A1 (en) | 1992-04-02 | 1993-10-14 | Smithkline Beecham Corporation | Compounds useful for treating allergic or inflammatory diseases |
DE69331265T2 (en) | 1992-04-02 | 2002-08-08 | Smithkline Beecham Corp., Philadelphia | COMPOUNDS FOR TREATING INFLAMMABLE DISEASES AND INHIBITING THE PRODUCTION OF TUMORNESCROSE FACTOR |
US5484926A (en) | 1993-10-07 | 1996-01-16 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors |
JPH0733729A (en) | 1993-07-26 | 1995-02-03 | Kirin Brewery Co Ltd | Production of n-cyano-n'-substituted-arylcarboxyimidamide compound |
DE59401923D1 (en) | 1993-11-02 | 1997-04-10 | Hoechst Ag | Substituted heterocyclic carboxylic acid amide esters, their preparation and their use as medicaments |
IL121789A (en) | 1996-10-03 | 2001-06-14 | Rohm & Haas | Pharmaceutical composition for inhibiting mammalian cell growth |
GB9622386D0 (en) | 1996-10-28 | 1997-01-08 | Sandoz Ltd | Organic compounds |
ZA979542B (en) | 1996-11-14 | 1998-05-12 | Rohm & Haas | Use of certain amides as probes for detection of antitubulin activity and residence monitoring. |
US6500405B1 (en) | 1996-11-14 | 2002-12-31 | Dow Agrosciences Llc | Use of certain amides as probes for detection of antitubulin activity and resistance monitoring |
JP4028014B2 (en) | 1996-12-25 | 2007-12-26 | 朝日化学工業株式会社 | Pickling accelerator, pickling composition containing pickling accelerator, and metal pickling method using the same |
US6333354B1 (en) | 1997-02-28 | 2001-12-25 | Byk Gulden Lomberg Chemische Fabrik Gmbh | Synergistic combination of PDE inhibitors and adenylate cyclase agonists or guanyl cyclyse agonists |
US6166037A (en) | 1997-08-28 | 2000-12-26 | Merck & Co., Inc. | Pyrrolidine and piperidine modulators of chemokine receptor activity |
CA2304503A1 (en) | 1997-09-23 | 1999-04-01 | Graham Johnson | Selective cpla2 inhibitors |
WO1999016766A1 (en) | 1997-10-01 | 1999-04-08 | Kyowa Hakko Kogyo Co., Ltd. | Benzodioxole derivatives |
US6362371B1 (en) | 1998-06-08 | 2002-03-26 | Advanced Medicine, Inc. | β2- adrenergic receptor agonists |
WO2000000531A1 (en) | 1998-06-30 | 2000-01-06 | The Dow Chemical Company | Polymer polyols and a process for the production thereof |
US6455603B1 (en) | 1998-06-30 | 2002-09-24 | Dow Global Technologies Inc. | Polymer polyols and a process for the production thereof |
GB9913083D0 (en) | 1999-06-04 | 1999-08-04 | Novartis Ag | Organic compounds |
US6391865B1 (en) | 1999-05-04 | 2002-05-21 | Schering Corporation | Piperazine derivatives useful as CCR5 antagonists |
WO2000066559A1 (en) | 1999-05-04 | 2000-11-09 | Schering Corporation | Piperidine derivatives useful as ccr5 antagonists |
JP3722700B2 (en) | 1999-05-04 | 2005-11-30 | シェーリング コーポレイション | Piperazine derivatives useful as CCR5 antagonists |
US6683115B2 (en) | 1999-06-02 | 2004-01-27 | Theravance, Inc. | β2-adrenergic receptor agonists |
ES2165768B1 (en) | 1999-07-14 | 2003-04-01 | Almirall Prodesfarma Sa | NEW DERIVATIVES OF QUINUCLIDINE AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM. |
US6660753B2 (en) | 1999-08-19 | 2003-12-09 | Nps Pharmaceuticals, Inc. | Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
CN1202865C (en) | 1999-08-21 | 2005-05-25 | 奥坦纳医药公司 | Synergistic combination |
PE20011010A1 (en) | 1999-12-02 | 2001-10-18 | Glaxo Group Ltd | OXAZOLES AND THIAZOLES REPLACED AS AGONIST OF THE RECEPTOR ACTIVATED BY THE HUMAN PEROXISOMAS PROLIFERATOR |
OA11558A (en) | 1999-12-08 | 2004-06-03 | Advanced Medicine Inc | Beta 2-adrenergic receptor agonists. |
US7300775B2 (en) | 1999-12-29 | 2007-11-27 | Verenium Corporation | Methods for producing α-substituted carboxylic acids using nitrilases and strecker reagents |
CA2405745A1 (en) | 2000-04-27 | 2001-11-08 | Boehringer Ingelheim Pharma Kg | New betamimetics having a long-lasting activity, processes for preparingthem and their use as medicaments |
UA72632C2 (en) | 2000-06-27 | 2005-03-15 | Лабораторіос С.А.Л.В.А.Т., С.А. | Carbamates, derivaties of arylalkylamines |
GB0015876D0 (en) | 2000-06-28 | 2000-08-23 | Novartis Ag | Organic compounds |
DE10038639A1 (en) | 2000-07-28 | 2002-02-21 | Schering Ag | New and known N-aryl 2-hydroxy-omega-arylalkanamide derivatives, useful e.g. for treating inflammatory diseases such as rheumatism |
ES2292604T5 (en) | 2000-08-05 | 2015-06-01 | Glaxo Group Limited | S-fluoromethyl ester of 6,9-difluoro-17 - [(2-furanylcarbonyl) oxy] -11-hydroxy-16-methyl-3-oxo-androsta-1,4-diene-17-carbotioic acid as an anti-inflammatory agent |
GB0028383D0 (en) | 2000-11-21 | 2001-01-03 | Novartis Ag | Organic compounds |
SI1345937T1 (en) | 2000-12-22 | 2006-02-28 | Almirall Prodesfarma Ag | Quinuclidine carbamate derivatives and their use as m3 antagonists |
JP4295985B2 (en) | 2000-12-28 | 2009-07-15 | ラボラトリオス・アルミラル・ソシエダッド・アノニマ | Novel quinuclidine derivative and pharmaceutical composition containing the same |
JP5025045B2 (en) | 2001-02-02 | 2012-09-12 | マルホ株式会社 | Enhancement of TIMP production by polysulfated polysaccharides |
PE20020870A1 (en) | 2001-02-13 | 2002-11-18 | Aventis Pharma Gmbh | 6,7,8,9-TETRAHYDRO-5H-BENZOCYCLOHEPTENYL ACILATED AMINES |
GB0103630D0 (en) | 2001-02-14 | 2001-03-28 | Glaxo Group Ltd | Chemical compounds |
DE60220887T2 (en) | 2001-03-08 | 2008-02-28 | Glaxo Group Ltd., Greenford | AGONISTS OF BETA ADRENORE RECEPTORS |
ATE381537T1 (en) | 2001-03-22 | 2008-01-15 | Glaxo Group Ltd | FORMANILIDE DERIVATIVES AS BETA2 ADRENORECEPTOR AGONISTS |
CA2445839A1 (en) | 2001-04-30 | 2002-11-07 | Glaxo Group Limited | Anti-inflammatory 17.beta.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.alpha |
US20040248867A1 (en) | 2001-06-12 | 2004-12-09 | Keith Biggadike | Novel anti-inflammatory 17.alpha.-heterocyclic-esters of 17.beta.carbothioate androstane derivatives |
EP2039762A3 (en) | 2001-06-21 | 2009-07-29 | Verenium Corporation | Nitralases |
SE0102438D0 (en) | 2001-07-05 | 2001-07-05 | Astrazeneca Ab | New compounds |
FR2827603B1 (en) | 2001-07-18 | 2003-10-17 | Oreal | COMPOUNDS DERIVED FROM DIAMINOPYRAZOLE SUBSTITUTED BY A HETEROAROMATIC RADICAL AND THEIR USE IN OXIDATION DYES OF KERATINIC FIBERS |
ES2438985T3 (en) | 2001-09-14 | 2014-01-21 | Glaxo Group Limited | Inhalation formulation comprising phenetanolamine derivatives for the treatment of respiratory diseases |
RU2004110717A (en) | 2001-10-17 | 2005-10-20 | Юсиби, С.А. (Be) | Quinuclidine derivatives, methods for their preparation and their use as both M2- and / or M3-muscarinic receptors |
GB0125259D0 (en) | 2001-10-20 | 2001-12-12 | Glaxo Group Ltd | Novel compounds |
AR037517A1 (en) | 2001-11-05 | 2004-11-17 | Novartis Ag | DERIVATIVES OF NAFTIRIDINES, A PROCESS FOR THE PREPARATION, PHARMACEUTICAL COMPOSITION AND THE USE OF THEM FOR THE PREPARATION OF A MEDICINAL PRODUCT FOR THE TREATMENT OF AN INFLAMMATORY DISEASE |
TWI249515B (en) | 2001-11-13 | 2006-02-21 | Theravance Inc | Aryl aniline beta2 adrenergic receptor agonists |
WO2003042160A1 (en) | 2001-11-13 | 2003-05-22 | Theravance, Inc. | Aryl aniline beta-2 adrenergic receptor agonists |
AU2002356759A1 (en) | 2001-12-01 | 2003-06-17 | Glaxo Group Limited | 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents |
RS52522B (en) | 2001-12-20 | 2013-04-30 | Chiesi Farmaceutici S.P.A. | 1-alkyl-1-azoniabicyclo/2.2.2./octane carbamate derivatives and their use as muscarinic receptor antagonists |
WO2003072592A1 (en) | 2002-01-15 | 2003-09-04 | Glaxo Group Limited | 17.alpha-cycloalkyl/cycloylkenyl esters of alkyl-or haloalkyl-androst-4-en-3-on-11.beta.,17.alpha.-diol 17.beta.-carboxylates as anti-inflammatory agents |
WO2003062259A2 (en) | 2002-01-21 | 2003-07-31 | Glaxo Group Limited | Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents |
GB0202216D0 (en) | 2002-01-31 | 2002-03-20 | Glaxo Group Ltd | Novel compounds |
GB0204719D0 (en) | 2002-02-28 | 2002-04-17 | Glaxo Group Ltd | Medicinal compounds |
US7335779B2 (en) | 2002-03-08 | 2008-02-26 | Quonova, Llc | Modulation of pathogenicity |
EA008830B1 (en) | 2002-03-26 | 2007-08-31 | Бёрингер Ингельхайм Фармасьютиклз, Инк. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
AU2003230700A1 (en) | 2002-03-26 | 2003-10-13 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
US7282591B2 (en) | 2002-04-11 | 2007-10-16 | Merck & Co., Inc. | 1h-benzo{f}indazol-5-yl derivatives as selective glucocorticoid receptor modulators |
ES2206021B1 (en) | 2002-04-16 | 2005-08-01 | Almirall Prodesfarma, S.A. | NEW DERIVATIVES OF PIRROLIDINIO. |
ES2298511T3 (en) | 2002-04-25 | 2008-05-16 | Glaxo Group Limited | DERIVATIVES OF PHENETHANOLAMINE. |
US7704995B2 (en) | 2002-05-03 | 2010-04-27 | Exelixis, Inc. | Protein kinase modulators and methods of use |
CA2484209C (en) | 2002-05-03 | 2013-06-11 | Exelixis, Inc. | Protein kinase modulators and methods of use |
WO2003099764A1 (en) | 2002-05-28 | 2003-12-04 | Theravance, Inc. | ALKOXY ARYL β2 ADRENERGIC RECEPTOR AGONISTS |
ES2201907B1 (en) | 2002-05-29 | 2005-06-01 | Almirall Prodesfarma, S.A. | NEW DERIVATIVES OF INDOLILPIPERIDINE AS POWERFUL ANTIHISTAMINIC AND ANTIALERGIC AGENTS. |
US7186864B2 (en) | 2002-05-29 | 2007-03-06 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
DE10224888A1 (en) | 2002-06-05 | 2003-12-24 | Merck Patent Gmbh | pyridazine |
US7074806B2 (en) | 2002-06-06 | 2006-07-11 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
DE10225574A1 (en) | 2002-06-10 | 2003-12-18 | Merck Patent Gmbh | New 1-acyl-3-phenyl-5,6-dihydro-4H-pyridazine derivatives, are phosphodiesterase IV inhibitors useful e.g. for treating asthma, allergy, inflammation, autoimmune diseases or myocardial diseases |
DE10227269A1 (en) | 2002-06-19 | 2004-01-08 | Merck Patent Gmbh | thiazole |
DE60312520T2 (en) | 2002-06-25 | 2007-11-22 | Merck Frosst Canada Ltd., Kirkland | 8- (biaryl) quinoline PDE4 INHIBITORS |
US20060004056A1 (en) | 2002-07-02 | 2006-01-05 | Bernard Cote | Di-aryl-substituted-ethan pyridone pde4 inhibitors |
ES2204295B1 (en) | 2002-07-02 | 2005-08-01 | Almirall Prodesfarma, S.A. | NEW DERIVATIVES OF QUINUCLIDINE-AMIDE. |
AU2003281355A1 (en) | 2002-07-08 | 2004-01-23 | Pfizer Products Inc. | Modulators of the glucocorticoid receptor |
GB0217225D0 (en) | 2002-07-25 | 2002-09-04 | Glaxo Group Ltd | Medicinal compounds |
US7186735B2 (en) | 2002-08-07 | 2007-03-06 | Sanofi-Aventis Deutschland Gmbh | Acylated arylcycloalkylamines and their use as pharmaceuticals |
US7338956B2 (en) | 2002-08-07 | 2008-03-04 | Sanofi-Aventis Deutschland Gmbh | Acylamino-substituted heteroaromatic compounds and their use as pharmaceuticals |
PE20050130A1 (en) | 2002-08-09 | 2005-03-29 | Novartis Ag | ORGANIC COMPOUNDS |
AU2003260371A1 (en) | 2002-08-10 | 2004-03-11 | Altana Pharma Ag | Piperidine-n-oxide-derivatives |
PL372926A1 (en) | 2002-08-10 | 2005-08-08 | Altana Pharma Ag | Piperidine-pyridazones and phthalazones as pde4 inhibitors |
WO2004018449A1 (en) | 2002-08-10 | 2004-03-04 | Altana Pharma Ag | Piperidine-derivatives as pde4 inhibitors |
CA2494650A1 (en) | 2002-08-10 | 2004-03-04 | Altana Pharma Ag | Pyridazinone-derivatives as pde4 inhibitors |
RS20050116A (en) | 2002-08-17 | 2007-11-15 | Altana Pharma Ag., | Novel phenanthridines |
JP2005537313A (en) | 2002-08-17 | 2005-12-08 | アルタナ ファルマ アクチエンゲゼルシャフト | New benzonaphthyridine |
WO2004018437A1 (en) | 2002-08-20 | 2004-03-04 | Neurogen Corporation | 5-substituted-2-arylpyrazines as modulators of crf receptors |
CA2496175A1 (en) | 2002-08-21 | 2004-03-04 | Boehringer Ingelheim Pharmaceuticals, Inc. | Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
SE0202483D0 (en) | 2002-08-21 | 2002-08-21 | Astrazeneca Ab | Chemical compounds |
US7288562B2 (en) | 2002-08-23 | 2007-10-30 | Ranbaxy Laboratories Limited | Fluoro and sulphonylamino containing 3,6-disubstituted azabicyclo (3.1.0) hexane derivatives as muscarinic receptor antagonists |
GB0219961D0 (en) | 2002-08-28 | 2002-10-02 | Pfizer Ltd | Oxytocin inhibitors |
BR0313923A (en) | 2002-08-29 | 2005-07-12 | Boehringer Ingelheim Pharma | 3- (Sulfonamidoethyl) indole derivatives for use as glucocorticoid mimetics in the treatment of inflammatory, allergic and proliferative diseases |
JP4587294B2 (en) | 2002-08-29 | 2010-11-24 | ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング | 2-hydroxy-6-phenylphenanthridine as PDE4 inhibitor |
DE60311662T2 (en) | 2002-08-29 | 2007-10-25 | Altana Pharma Ag | 3-HYDROXY-6-PHENYLPHENANTHRIDINE AS PDE-4 INHIBITORS |
GB0220730D0 (en) | 2002-09-06 | 2002-10-16 | Glaxo Group Ltd | Medicinal compounds |
JP2006096662A (en) | 2002-09-18 | 2006-04-13 | Sumitomo Pharmaceut Co Ltd | New 6-substituted urasil derivative, and therapeutic agent for allergic disease |
JPWO2004026873A1 (en) | 2002-09-18 | 2006-01-19 | 小野薬品工業株式会社 | Triazaspiro [5.5] undecane derivatives and drugs containing them as active ingredients |
JP2004107299A (en) | 2002-09-20 | 2004-04-08 | Japan Energy Corp | New 1-substituted urasil derivative and therapeutic agent for allergic disease |
CA2499150A1 (en) | 2002-09-20 | 2004-04-01 | Merck & Co., Inc. | Octahydro-2-h-naphtho[1,2-f] indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators |
DE10246374A1 (en) | 2002-10-04 | 2004-04-15 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | New 4-(2-alkylamino-1-hydroxyethyl)-3-alkoxy-benzene-1,2-diol derivatives, are beta-mimetics having a long duration of action, useful e.g. for treating asthma, chronic obstructive pulmonary disease or arrhythmia |
US6951888B2 (en) | 2002-10-04 | 2005-10-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Betamimetics with a prolonged duration of activity, processes for preparing them, and their use as pharmaceutical compositions |
EP1440966A1 (en) | 2003-01-10 | 2004-07-28 | Pfizer Limited | Indole derivatives useful for the treatment of diseases |
US6844362B2 (en) | 2002-10-11 | 2005-01-18 | Pfizer Inc | Indole derivatives useful for the treatment of diseases |
AU2003269316A1 (en) | 2002-10-11 | 2004-05-04 | Pfizer Inc. | Indole derivatives as beta-2 agonists |
ES2291733T3 (en) | 2002-10-22 | 2008-03-01 | Glaxo Group Limited | MEDICAL ARYLETHANOLAMINE COMPOUNDS. |
AU2003269317B2 (en) | 2002-10-23 | 2009-10-29 | Glenmark Pharmaceuticals Ltd. | Novel tricyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them |
NZ539676A (en) | 2002-10-28 | 2006-10-27 | Glaxo Group Ltd | Phenethanolamine derivative for the treatment of respiratory diseases |
GB0225030D0 (en) | 2002-10-28 | 2002-12-04 | Glaxo Group Ltd | Medicinal compounds |
GB0225287D0 (en) | 2002-10-30 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
GB0225535D0 (en) | 2002-11-01 | 2002-12-11 | Glaxo Group Ltd | Medicinal compounds |
GB0225540D0 (en) | 2002-11-01 | 2002-12-11 | Glaxo Group Ltd | Medicinal compounds |
US7056916B2 (en) | 2002-11-15 | 2006-06-06 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Medicaments for the treatment of chronic obstructive pulmonary disease |
DE10253282A1 (en) | 2002-11-15 | 2004-05-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Treatment of chronic obstructive pulmonary disease, using new or known N-substituted 2-amino-1-(benz-(1,4)-oxazin-3-on-8-yl)-ethanol derivative beta-mimetic agents, suitable for once-daily administration |
DE10253220A1 (en) | 2002-11-15 | 2004-05-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | New 2-(N-phenylalkyl-amino)-1-phenyl-ethanol derivatives, are beta-adrenergic agents especially useful for treating inflammatory and obstructive respiratory diseases such as asthma or COPD |
DE10253426B4 (en) | 2002-11-15 | 2005-09-22 | Elbion Ag | Novel hydroxyindoles, their use as inhibitors of phosphodiesterase 4 and methods for their preparation |
DE10261874A1 (en) | 2002-12-20 | 2004-07-08 | Schering Ag | Nonsteroidal anti-inflammatories |
CA2512987C (en) | 2003-01-21 | 2011-06-14 | Merck & Co., Inc. | 17-carbamoyloxy cortisol derivatives as selective glucocorticoid receptor modulators |
PE20040950A1 (en) | 2003-02-14 | 2005-01-01 | Theravance Inc | BIPHENYL DERIVATIVES AS AGONISTS OF ß2-ADRENERGIC RECEPTORS AND AS ANTAGONISTS OF MUSCARINAL RECEPTORS |
JP2007524596A (en) | 2003-02-28 | 2007-08-30 | トランスフォーム・ファーマシューティカルズ・インコーポレイテッド | Co-crystal pharmaceutical composition |
GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
EP1460064A1 (en) | 2003-03-14 | 2004-09-22 | Pfizer Limited | Indole-2-carboxamide derivatives useful as beta-2 agonists |
AU2004240586A1 (en) | 2003-05-15 | 2004-12-02 | Merck & Co., Inc. | 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as S1P receptor agonists |
GB0312832D0 (en) | 2003-06-04 | 2003-07-09 | Pfizer Ltd | 2-amino-pyridine derivatives useful for the treatment of diseases |
US7375100B2 (en) | 2003-06-04 | 2008-05-20 | Pfizer Inc | 2-amino-pyridine derivatives useful for the treatment of diseases |
US20060241288A1 (en) | 2003-06-10 | 2006-10-26 | Ace Biosciences A/S | Extracellular aspergillus polypeptides |
EP1636269A2 (en) | 2003-06-10 | 2006-03-22 | Ace Biosciences A/S | Extracellular aspergillus polypeptides |
GB0321710D0 (en) | 2003-09-16 | 2003-10-15 | Novartis Ag | Organic compounds |
MXPA06007640A (en) | 2004-01-12 | 2007-04-17 | Cytopia Res Pty Ltd | Selective kinase inhibitors. |
WO2005072681A2 (en) | 2004-01-23 | 2005-08-11 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments of inflammatory and neurotic pain. |
WO2005079802A1 (en) | 2004-02-12 | 2005-09-01 | Merck & Co., Inc. | Bipyridyl amides as modulators of metabotropic glutamate receptor-5 |
KR20070030196A (en) | 2004-04-13 | 2007-03-15 | 이카겐, 인코포레이티드 | Polycyclic pyridines as potassium ion channel modulators |
WO2006053109A1 (en) | 2004-11-10 | 2006-05-18 | Synta Pharmaceuticals Corp. | Heteroaryl compounds |
WO2006065721A2 (en) | 2004-12-13 | 2006-06-22 | Enanta Pharmaceuticals, Inc. | 11, 12-lactone bicyclolides |
TW200635899A (en) | 2004-12-22 | 2006-10-16 | Astrazeneca Ab | Chemical compounds |
AU2005317870A1 (en) | 2004-12-22 | 2006-06-29 | Astrazeneca Ab | Pyridine carboxamide derivatives for use as anticancer agents |
WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
CN101849943A (en) | 2005-06-06 | 2010-10-06 | 菲布罗根公司 | Use the improved treatment for anemia of HIF alpha stabilizers |
US20090017006A1 (en) | 2005-07-06 | 2009-01-15 | Biodevelops Pharma Entwicklung Gmbh | Use of a compound for enhancing the expression of membrane proteins on the cell surface |
SI2774925T1 (en) | 2005-11-08 | 2017-04-26 | Vertex Pharmaceuticals Incorporated | Heterocyclic modulators of ATP-binding cassette transporters |
US7678818B2 (en) | 2006-02-07 | 2010-03-16 | Hoffmann-La Roche Inc. | Anthranilamide and 2-amino-heteroarene-carboxamide compounds |
CA2637768C (en) | 2006-02-07 | 2014-07-29 | F. Hoffmann-La Roche Ag | Benzamide and heteroarene derivatives |
IN2014CN04406A (en) | 2006-03-30 | 2015-09-04 | Ptc Therapeutics Inc | |
US20100022547A1 (en) | 2006-06-02 | 2010-01-28 | Brandeis University | Compounds and Methods for Treating Mammalian Gastrointestinal Parasitic Infections |
US20080027044A1 (en) | 2006-06-13 | 2008-01-31 | Kim Lewis | Prodrug antibiotic screens |
WO2008002671A2 (en) | 2006-06-29 | 2008-01-03 | Alantos Pharmaceuticals Holding, Inc. | Metalloprotease inhibitors |
CA2658096A1 (en) | 2006-07-19 | 2008-01-24 | Osurf (Ohio State University Research Foundation) | Selective androgen receptor modulators, analogs and derivatives thereof and uses thereof |
SI2848610T1 (en) | 2006-11-15 | 2018-02-28 | Ym Biosciences Australia Pty Ltd | Inhibitors of kinase activity |
CA2672940A1 (en) | 2006-12-20 | 2008-07-10 | Schering Corporation | Novel jnk inhibitors |
DE102007017884A1 (en) | 2007-04-13 | 2008-10-16 | Grünethal GmbH | Novel vanilloid receptor ligands and their use in the preparation of medicines |
US7928111B2 (en) | 2007-06-08 | 2011-04-19 | Senomyx, Inc. | Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors |
AR067585A1 (en) | 2007-07-19 | 2009-10-14 | Schering Corp | AMIDAS HETEROCICLICAL COMPOUNDS AS INHIBITORS OF PROTEINCINASE |
EP2203436A1 (en) | 2007-09-17 | 2010-07-07 | Neurosearch A/S | Pyrazine derivatives and their use as potassium channel modulators |
JP5583592B2 (en) | 2007-11-30 | 2014-09-03 | ニューリンク ジェネティクス コーポレイション | IDO inhibitor |
CN101925603B (en) | 2007-12-13 | 2013-12-04 | 沃泰克斯药物股份有限公司 | Modulators of cystic fibrosis transmembrane conductance regulator |
EP2271622B1 (en) | 2008-02-28 | 2017-10-04 | Vertex Pharmaceuticals Incorporated | Heteroaryl derivatives as CFTR Modulators |
US8268834B2 (en) | 2008-03-19 | 2012-09-18 | Novartis Ag | Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme |
HUE026220T2 (en) * | 2008-03-31 | 2016-05-30 | Vertex Pharma | Pyridyl derivatives as CFTR modulators |
JP2011520831A (en) | 2008-05-13 | 2011-07-21 | ノバルティス アーゲー | 3,5-Diamino-6-chloro-pyrazine-2-carboxylic acid derivatives and their use as epithelial sodium channel blockers for the treatment of airway diseases |
CN102112130A (en) * | 2008-06-10 | 2011-06-29 | 诺瓦提斯公司 | Pyrazine derivatives as epithelial sodium channel blockers |
HUE031419T2 (en) | 2008-07-03 | 2017-07-28 | Astellas Pharma Inc | Triazole derivative or salt thereof |
CA2641297A1 (en) | 2008-07-11 | 2010-01-11 | Richard B. Dorshow | Pyrazine derivatives, methods of use, and methods for preparing same |
US8518952B2 (en) | 2008-08-06 | 2013-08-27 | Pfizer Inc. | 6 substituted 2-heterocyclylamino pyrazine compounds as CHK-1 inhibitors |
US8372885B2 (en) | 2008-09-17 | 2013-02-12 | Novartis Ag | Organic compounds and their uses |
CN102271682B (en) | 2008-10-31 | 2015-12-16 | 默沙东公司 | Be used for the treatment of the P2X of pain 3receptor antagonist |
US8513242B2 (en) | 2008-12-12 | 2013-08-20 | Cystic Fibrosis Foundation Therapeutics, Inc. | Pyrimidine compounds and methods of making and using same |
EP2202232A1 (en) | 2008-12-26 | 2010-06-30 | Laboratorios Almirall, S.A. | 1,2,4-oxadiazole derivatives and their therapeutic use |
EP2382197B1 (en) | 2008-12-30 | 2016-10-05 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
US7928105B2 (en) | 2009-01-23 | 2011-04-19 | Takeda Pharmaceutical Company Limited | Substituted 6a,7,8,9-tetrahydropyrido[3,2-e]pyrrolo[1,2-a]pyrazin-6(5H)-ones |
JP2012051807A (en) | 2009-02-26 | 2012-03-15 | Eisai R & D Management Co Ltd | Arylimidazole compound |
WO2010117662A1 (en) | 2009-03-30 | 2010-10-14 | Exelixis, Inc. | Modulators of s1p and methods of making and using |
TW201103904A (en) | 2009-06-11 | 2011-02-01 | Hoffmann La Roche | Janus kinase inhibitor compounds and methods |
WO2010151747A1 (en) | 2009-06-26 | 2010-12-29 | Cystic Fibrosis Foundation Therapeutics, Inc. | Pyrimine compounds and methods of making and using same |
JP2012180281A (en) | 2009-06-29 | 2012-09-20 | Dainippon Sumitomo Pharma Co Ltd | New oxadiazole derivative |
WO2011008931A2 (en) | 2009-07-15 | 2011-01-20 | Cystic Fibrosis Foundation Therapeutics, Inc. | Arylpyrimidine compounds and combination therapy comprising same for treating cystic fibrosis & related disorders |
US8415381B2 (en) | 2009-07-30 | 2013-04-09 | Novartis Ag | Heteroaryl compounds and their uses |
US8247436B2 (en) * | 2010-03-19 | 2012-08-21 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of CF |
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